Design, synthesis, and biological evaluation of novel 1, 2, 4-triazole derivatives as antifungal agent

被引：11

作者：

Chai, Xiaoyun ^{[1
]}

Yu, Shichong ^{[1
]}

Jiang, Yongwei ^{[1
]}

Zou, Yan ^{[1
]}

Wu, Qiuye ^{[1
]}

Zhang, Dazhi ^{[1
]}

Jiang, Yuanying ^{[2
]}

Cao, Yongbing ^{[2
]}

Sun, Qingyan ^{[1
]}

机构：

[1] Second Mil Med Univ, Sch Pharm, Dept Organ Chem, Shanghai 200433, Peoples R China

[2] Second Mil Med Univ, Sch Pharm, Drug Res Ctr, Shanghai 200433, Peoples R China

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2012年 / 35卷 / 11期

基金：

中国国家自然科学基金;

关键词：

Triazole; Synthesis; Antifungal activity; CACYP51; Molecular docking; TRIAZOLE DERIVATIVES; ASPERGILLOSIS;

D O I：

10.1007/s12272-012-1105-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 1, 2, 4-triazole derivatives (9a-p) have been designed and synthesized as the potential antifungal agents. All compounds were characterized by H-1-NMR, C-13-NMR, and LCMS. Their antifungal activities against seven human pathogenic fungi were evaluated in vitro by measuring the minimal inhibitory concentrations. Most of the tested compounds were found to be more potent against Candida albicans than the control drug fluconazole.

引用

页码：1895 / 1901

页数：7

共 16 条

[1]

[Anonymous], 2002, CLSI document M27-A2, V2nd

[2]

[Anonymous], 2010, EUR J MED CHEM, DOI DOI 10.1016/j.ejmech.2010.07.002

[3] New azoles with antifungal activity: Design, synthesis, and molecular docking [J].

Chai, Xiaoyun ;

Zhang, Jun ;

Cao, Yongbing ;

Zou, Yan ;

Wu, Qiuye ;

Zhang, Dazhi ;

Jiang, Yuanying ;

Sun, Qingyan .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (02) :686-689

[4] Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14α-demethylase [J].

Chai, Xiaoyun ;

Zhang, Jun ;

Hu, Honggang ;

Yu, Shichong ;

Sun, Qingyan ;

Dan, Zhigang ;

Jiang, Yuanying ;

Wu, Qiuye .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (05) :1913-1920

[5] ANALOGS OF NUCLEOSIDES .43. PREPARATION OF RIBOSYL DERIVATIVES OF 1,2,4-TRIAZOL-3(2H)-ONE AND 5-METHYL-1,2,4-TRIAZOL-3(2H)-ONE [J].

HREBABECKY, H ;

BERANEK, J .

COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, 1985, 50 (03) :779-788

[6] Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents [J].

Jiang, Yongwei ;

Zhang, Jun ;

Cao, Yongbing ;

Chai, Xiaoyun ;

Zou, Yan ;

Wu, Qiuye ;

Zhang, Dazhi ;

Jiang, Yuanying ;

Sun, Qingyan .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (15) :4471-4475

[7] Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one [J].

Jiang, Yongwei ;

Cao, Yongbin ;

Zhang, Jun ;

Zou, Yan ;

Chai, Xiaoyun ;

Hu, Honggang ;

Zhao, Qingjie ;

Wu, Qiuye ;

Zhang, Dazhi ;

Jiang, Yuanying ;

Sun, Qingyan .

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (07) :3135-3141

[8]

Krishnamurthy N., 1998, US Patent, Patent No. 5728834

[9] History of the development of azole derivatives [J].

Maertens, JA .

CLINICAL MICROBIOLOGY AND INFECTION, 2004, 10 :1-10

[10] EPIDEMIOLOGY AND ANTIFUNGAL RESISTANCE IN INVASIVE ASPERGILLOSIS ACCORDING TO PRIMARY DISEASE - REVIEW OF THE LITERATURE [J].

Mayr, A. ;

Lass-Floerl, C. .

EUROPEAN JOURNAL OF MEDICAL RESEARCH, 2011, 16 (04) :153-157

← 1 2 →